Design, synthesis and biological evaluation of novel DPP-IV inhibitors

被引：0

作者：

Karelia, Chirag ^{[1
]}

Parmar, Kailash ^{[1
]}

Teli, Divya ^{[1
]}

Chhabria, Mahesh ^{[1
]}

机构：

[1] LM Coll Pharm, Dept Pharmaceut Chem, Ahmadabad 380009, Gujarat, India

来源：

JOURNAL OF THE INDIAN CHEMICAL SOCIETY | 2020年 / 97卷 / 08期

关键词：

Type; 2; diabetes; DPP-IV inhibitor; 3D QSAR pharmacophore; virtual screening; S; N-acetal; N; DERIVATIVES;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Diabetes mellitus is one of the top ten leading causes of death worldwide. DPP-IV inhibition became an attractive target in controlling type 2 diabetes. Because of the several adverse effects associated with current DPP-IV inhibitors, the discovery and development of newer DPP-IV inhibitors are crucial. Ligand-based 3D QSAR pharmacophore modeling method was used in recognizing the important molecular chemical features of potent DPP-IV inhibitors. The best pharmacophore model (Hypo 1) was generated using HypoGen algorithm of Discovery Studio 2.1 (DS). Based on the Hypo 1 model, four novel designed compounds were synthesized, characterized and screened for their DPP-IV inhibitory potentials. All the compounds (9), (10), (11) and (12) showed IC50 values ranging from 0.035-0.35 mu M.

引用

页码：1227 / 1235

页数：9

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